Comparative Pharmacology
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE versus EMTRICITABINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DOLUTEGRAVIR LAMIVUDINE TENOFOVIR DISOPROXIL FUMARATE versus EMTRICITABINE.
DOLUTEGRAVIR; LAMIVUDINE; TENOFOVIR DISOPROXIL FUMARATE vs EMTRICITABINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dolutegravir is an HIV-1 integrase strand transfer inhibitor (INSTI) that blocks the integration of HIV-1 DNA into host genomic DNA. Lamivudine and tenofovir disoproxil fumarate are nucleoside reverse transcriptase inhibitors (NRTIs) that inhibit HIV-1 reverse transcriptase by competing with natural substrates and causing chain termination.
Nucleoside reverse transcriptase inhibitor; phosphorylated to emtricitabine triphosphate which competes with endogenous deoxycytidine triphosphate and incorporates into viral DNA causing chain termination.
One tablet orally once daily containing dolutegravir 50 mg, lamivudine 300 mg, and tenofovir disoproxil fumarate 300 mg.
200 mg orally once daily, typically in combination with other antiretroviral agents.
None Documented
None Documented
Clinical Note
moderateEmtricitabine + Ribavirin
"Emtricitabine may increase the hepatotoxic activities of Ribavirin."
Clinical Note
moderateLamivudine + Emtricitabine
"The risk or severity of adverse effects can be increased when Lamivudine is combined with Emtricitabine."
Clinical Note
moderateGanciclovir + Emtricitabine
"The risk or severity of adverse effects can be increased when Ganciclovir is combined with Emtricitabine."
Clinical Note
moderateValganciclovir + Emtricitabine
Dolutegravir: ~14 hours (range 11-18) in HIV-1-infected adults, supports once-daily dosing. Lamivudine: ~18-19 hours in HIV-infected adults, allows once-daily dosing; prolonged in renal impairment. Tenofovir disoproxil fumarate: ~17 hours (tenofovir) in HIV-infected adults, supports once-daily dosing; extended in renal impairment.
Terminal elimination half-life is approximately 10 hours (range 8–12 hours) in adults with normal renal function; prolonged to >20 hours in severe renal impairment (CrCl <30 mL/min).
Dolutegravir: ~64% feces (as unchanged drug), 31% urine (as unchanged and metabolites). Lamivudine: ~70% urine (as unchanged drug) via active tubular secretion, ~6% as inactive trans-sulfoxide metabolite. Tenofovir disoproxil fumarate: ~70-80% urine (as unchanged tenofovir) via glomerular filtration and active tubular secretion.
Renal: approximately 86% of the dose is excreted unchanged in urine via glomerular filtration and active tubular secretion. Biliary/fecal: minimal (<14% as unchanged drug and metabolites in feces).
Category A/B
Category C
NRTI
Antiretroviral, NRTI
"The risk or severity of adverse effects can be increased when Valganciclovir is combined with Emtricitabine."